JP2022109243A - メシル酸ナファモスタットの共結晶多形及びその製造方法 - Google Patents

メシル酸ナファモスタットの共結晶多形及びその製造方法 Download PDF

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JP2022109243A
JP2022109243A JP2022004094A JP2022004094A JP2022109243A JP 2022109243 A JP2022109243 A JP 2022109243A JP 2022004094 A JP2022004094 A JP 2022004094A JP 2022004094 A JP2022004094 A JP 2022004094A JP 2022109243 A JP2022109243 A JP 2022109243A
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Japan
Prior art keywords
nafamostat mesylate
crystal
acid
nafamostat
mesylate
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JP2022004094A
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English (en)
Japanese (ja)
Inventor
ジュ パク，ウン
Eun Ju Park
ジ，ヒョン
Hyun Ji
オ パク，ジン
Jin Oh Park
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Daebong LS Co Ltd
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Daebong LS Co Ltd
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Publication of JP2022109243A publication Critical patent/JP2022109243A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C277/06—Purification or separation of guanidine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Analytical Chemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2022004094A 2021-01-14 2022-01-14 メシル酸ナファモスタットの共結晶多形及びその製造方法 Pending JP2022109243A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020210005551A KR102288679B1 (ko) 2021-01-14 2021-01-14 메실산 나파모스타트의 공결정다형 및 그의 제조방법
KR10-2021-0005551 2021-01-14

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Publication Number Publication Date
JP2022109243A true JP2022109243A (ja) 2022-07-27

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JP (1) JP2022109243A (ko)
KR (1) KR102288679B1 (ko)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004231598A (ja) * 2003-01-31 2004-08-19 Shizuoka Coffein Co Ltd メシル酸ナファモスタットの結晶多形及びその製造方法
JP2007516259A (ja) * 2003-12-09 2007-06-21 メッドクリスタルフォームズ、エルエルシー 活性剤との混合相共結晶の調製方法
JP2012087099A (ja) * 2010-10-21 2012-05-10 Katsura Chemical Co Ltd ナファモスタットメシル酸塩の晶析方法
WO2014007326A1 (ja) * 2012-07-04 2014-01-09 味の素株式会社 ナファモスタットメシル酸塩の製造方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5753454A (en) 1980-09-16 1982-03-30 Torii Yakuhin Kk Guanidinobenzoate and anticomplementary agent
JP4251892B2 (ja) * 2003-03-20 2009-04-08 関東化学株式会社 ４−グアニジノ安息香酸またはその誘導体のエステル化方法
DE102008028071A1 (de) * 2008-06-12 2009-12-17 Bayer Schering Pharma Aktiengesellschaft Neue Cokristall-Verbindung von Rivaroxaban und Malonsäure
KR20160017798A (ko) * 2014-08-05 2016-02-17 대화제약 주식회사 타달라필 공결정 및 이의 제조방법

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004231598A (ja) * 2003-01-31 2004-08-19 Shizuoka Coffein Co Ltd メシル酸ナファモスタットの結晶多形及びその製造方法
JP2007516259A (ja) * 2003-12-09 2007-06-21 メッドクリスタルフォームズ、エルエルシー 活性剤との混合相共結晶の調製方法
JP2012087099A (ja) * 2010-10-21 2012-05-10 Katsura Chemical Co Ltd ナファモスタットメシル酸塩の晶析方法
WO2014007326A1 (ja) * 2012-07-04 2014-01-09 味の素株式会社 ナファモスタットメシル酸塩の製造方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
山下博之: "医薬品原薬における共結晶形成と熱挙動", NETSU SOKUTEI, vol. 42(1), JPN7023000026, 2015, pages 17 - 24, ISSN: 0004966439 *
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0004966438 *

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